Cisapride (Propulsid, Alimix, Propulsin, Enteropride, Kinestase) acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic.
Cisapride inhibits vascular Kv current independently of serotonin 5-HT4-receptor activation[2]. As HERG channel blocker, cisapride, can inhibit the growth of gastric cancer cells by altering distribution of cell cycle and inducing apoptosis so as to be of potential value in the treatment of gastric cancer. Cisapride could inhibit the growth and clonogenicity of human gastric cancer lines by specific blockage of HERG channel in a time- and dose-dependent manner while has little effects on GES cells[3].
Cisapride is widely prescribed for the treatment of gastrointestinal motility dysfunctions, such as gastroesophageal reflux disorder (GERD), chronic intestinal pseudo-obstruction, and slow-transit constipation gastroparesis. Although cisapride is a beneficial prokinetic agent, several common side effects, such as abdominal pain, nausea, diarrhea, and increased frequency of urination, have been reported[2]. In rat, the PK profile indicate the T1/2 for cisapride is 1.48 h[1].
[1] Park JS, et al. Eur J Med Chem. 2016, 109:75-88. [2] Kim HW, et al.Biochem Biophys Res Commun. 2016, 478(3):1423-8. [3] Shao XD, et al. Cancer Biol Ther. 2005, 4(3):295-301.